Background:
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10?μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
Loureirin B enhances the relative mRNA level of Pdx-1 and MafA. Loureirin B (1, 0.1, and 0.01?μM) increases insulin secretion in Ins-1 cells. Loureirin B (0.01?μM) almost causes no toxicity on cells. Loureirin B improves the level of expressions of MafA and Pdx-1 and ATP level. Loureirin B inhibits the KATP current but increases the [Ca2+]i level in Ins-1 cells[1]. Loureirin B inhibits the expression of Col1 and FN, as well as the TGF-β1-mediated up regulation of p-JNK. Loureirin B also inhibits the up regulation of p-ERK that is induced by TGF-β1. Moreover, Loureirin B inhibits the contraction of TGF-β1-stimulated fibroblasts through the down regulation of p-ERK and p-JNK. However, Loureirin B does not suppress the up regulation of p-p38 that is induced by TGF-β1[2]. Loureirin B downregulates both mRNA and protein levels of type I collagen, type III collagen and α-smooth muscle actin in a dose dependent manner in HS fibroblasts. Loureirin B also suppresses fibroblast proliferative activity and redistributes cell cycle, but does not affect cell apoptosis[3].
Loureirin B significantly improves the arrangement and deposition of collagen fibres, decreases protein levels of ColI, ColIII and α-SMA and suppresses myofibroblast differentiation and scar proliferative activity, in a rabbit ear scar model. Loureirin B effectively inhibits TGF-β1-induced upregulation of ColI, ColIII and α-SMA levels, myofibroblast differentiation and the activation of Smad2 and Smad3, in NS fibroblasts[3].
参考文献:
[1]. Sha Y, et al. Loureirin B promotes insulin secretion through inhibition of KATP channel and influx of intracellular calcium. J Cell Biochem. 2017 Aug 17.
[2]. He T, et al. Loureirin B Inhibits Hypertrophic Scar Formation via Inhibition of the TGF-β1-ERK/JNK Pathway. Cell Physiol Biochem. 2015;37(2):666-76.
[3]. Bai X, et al. Loureirin B inhibits fibroblast proliferation and extracellular matrix deposition in hypertrophic scar via TGF-β/Smad pathway. Exp Dermatol. 2015 May;24(5):355-60.
[4]. Yu Jiang, et al. Bioactivity-Guided Fractionation of the Traditional Chinese Medicine Resina Draconis Reveals Loureirin B as a PAI-1 Inhibitor. Evidence-Based Complementary and Alternative Medicine
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